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A68930 is a potent, full agonist at dopamine 1 (D 1 ) receptors in renal epithelial LLC‐PK 1 cells
Author(s) -
Grenader Arcady,
Healy Dennis P.
Publication year - 1992
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1992.tb14320.x
Subject(s) - fenoldopam , agonist , sch 23390 , chemistry , dopamine , adenosine , dopamine agonist , dopamine receptor d1 , medicine , partial agonist , endocrinology , dopamine receptor , receptor , stimulation , pharmacology , biology , biochemistry
The selective dopamine 1 (D 1 ) receptor agonists SK&F 82526 (fenoldopam) and A68930 and the mixed D 1 /D 2 agonist SK&F 85174 were tested for their ability to stimulate adenosine 3′:5′‐cyclic monophosphate (cyclic AMP) accumulation in the porcine renal epithelial cell line, LLC‐PK 1 . SK&F 82526 and SK&F 85174 were potent stimulators of cyclic AMP accumulation (EC 50 s 21.4 and 14.5 n m , respectively), but only partial agonists (intrinsic activities 31% and 46% of dopamine respectively). In contrast, A68930 was a potent, full agonist (EC50 12.7 n m , intrinsic activity 102% of dopamine). The stimulatory effects of A68930 and dopamine on cyclic AMP accumulation were not additive, and the stimulation of cyclic AMP accumulation by A68930 was blocked by the D 1 ‐selective antagonist, SCH 23390. These properties of A68930 suggest that it may be a useful D 1 ‐selective agonist to study renal D 1 receptor mechanisms in vitro and in vivo .